Cytarabine
(Synonyms: 阿糖胞苷; Cytosine β-D-arabinofuranoside; Cytosine Arabinoside; Ara-C) 目录号 : GC13070
Cytarabine（Ara-C）是一种胞嘧啶类似物，主要抑制DNA聚合酶的功能来阻断DNA合成。
Cas No.:147-94-4
Sample solution is provided at 25 µL, 10mM.
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| Cell experiment [1]: | |
Cell lines | P493-6、PrEC-LHS、RWPE cells |
Preparation Method | Cells were treated with doses of 0 to 656μM cytarabine, solubilized in water. Cell viability was determined 48h later. |
Reaction Conditions | 0-656µM; 48h |
Applications | P493-6 and PrEC-LHS cells showed high sensitivity to cytarabine only in the high MYC state. RWPE cells showed high sensitivity to cytarabine in both the low MYC state and the high MYC state. |
| Animal experiment [2]: | |
Animal models | Immune-competent mouse model of acute myeloid leukemia (AML) |
Preparation Method | Leukemic cells were injected into the tail vein of each mouse. Mice succumbed to AML development in an average of 31, 32 or 38 days depending on the injected subclone(s). Cytarabine was administered at different doses (100 or 200 mg/kg) intraperitoneally daily to each mouse. Mice were monitored for survival or euthanized whenever they presented the first signs of distress due to AML disease. |
Dosage form | 100、200mg/kg; i.p. |
Applications | Administration of cytarabine significantly improved mouse survival from 20% to 59.3%. |
References: [1] Chen W, Mou K Y, Solomon P, et al. Large remodeling of the Myc-induced cell surface proteome in B cells and prostate cells creates new opportunities for immunotherapy[J]. Proceedings of the National Academy of Sciences, 2021, 118(4): e2018861118. [2]Mopin A, Leprêtre F, Sebda S, et al. Detection of residual and chemoresistant leukemic cells in an immune-competent mouse model of acute myeloid leukemia: Potential for unravelling their interactions with immunity[J]. Plos one, 2022, 17(4): e0267508. | |
Cytarabine (Ara-C) is a cytosine analog that primarily inhibits the function of DNA polymerase to block DNA synthesis[1]. Cytarabine is an antimetabolite and antitumor drug belonging to the anthracycline class of drugs, mainly used to treat acute myeloid leukemia (AML), acute lymphoblastic leukemia (ALL) and lymphoma[2]. Cytarabine can affect the cell cycle and cause S phase cell arrest[3].
In vitro, P493-6, PrEC-LHS, and RWPE cells were treated with Cytarabine (0-656µM) for 48h. P493-6 and PrEC-LHS cells only showed drug sensitivity when MYC (a transcription factor) levels were high, while RWPE cells showed no effect on MYC status[4]. Cytarabine (100, 500nM) was used to treat Kasumi-3 and U937 cells with knockdown of FHL1 expression for 72h, which had a significant cell killing effect[5].
In vivo, cytarabine (200 mg/kg) was administered intraperitoneally to treat acute myeloid leukemia model mice, which significantly increased the survival rate of mice from 20% to 59.3%. The residual leukemia cells after treatment showed chemoresistance[6]. Cytarabine (10 mg/kg) was injected intravenously to treat AML model mice, which significantly improved the survival rate of mice，combined with decitabine can enhance the therapeutic effect[7].
References:
[1] Zhuo M, Gorgun M F, Englander E W. Neurotoxicity of cytarabine (Ara-C) in dorsal root ganglion neurons originates from impediment of mtDNA synthesis and compromise of mitochondrial function[J]. Free Radical Biology and Medicine, 2018, 121: 9-19.
[2] Di Francia R, Crisci S, De Monaco A, et al. Response and toxicity to cytarabine therapy in leukemia and lymphoma: from dose puzzle to pharmacogenomic biomarkers[J]. Cancers, 2021, 13(5): 966.
[3] van Pelt K, de Haan G, Vellenga E, et al. Administration of low-dose cytarabine results in immediate S-phase arrest and subsequent activation of cell cycling in murine stem cells[J]. Experimental hematology, 2005, 33(2): 226-231.
[4] Chen W, Mou K Y, Solomon P, et al. Large remodeling of the Myc-induced cell surface proteome in B cells and prostate cells creates new opportunities for immunotherapy[J]. Proceedings of the National Academy of Sciences, 2021, 118(4): e2018861118.
[5] Fu Y, Xu M, Cui Z, et al. Genome-wide identification of FHL1 as a powerful prognostic candidate and potential therapeutic target in acute myeloid leukaemia[J]. EBioMedicine, 2020, 52.
[6] Mopin A, Leprêtre F, Sebda S, et al. Detection of residual and chemoresistant leukemic cells in an immune-competent mouse model of acute myeloid leukemia: Potential for unravelling their interactions with immunity[J]. Plos one, 2022, 17(4): e0267508.
[7] Jing Y, Jin X, Wang L, et al. Decitabine-based chemotherapy followed by haploidentical lymphocyte infusion improves the effectiveness in elderly patients with acute myeloid leukemia[J]. Oncotarget, 2017, 8(32): 53654.
Cytarabine（Ara-C）是一种胞嘧啶类似物，主要抑制DNA聚合酶的功能来阻断DNA合成[1]。Cytarabine是一种抗代谢药和抗肿瘤药，属于蒽环类药物，主要用于治疗急性髓系白血病（AML）、急性淋巴细胞白血病（ALL）和淋巴瘤[2]。Cytarabine能够影响细胞周期，可引起S期细胞阻滞[3]。
在体外，Cytarabine（0-656µM）处理P493-6、PrEC-LHS、RWPE细胞48h， P493-6和PrEC-LHS细胞仅在MYC（一种转录因子）水平较高的状态下产生药物敏感性，而RWPE细胞对Cytarabine的敏感性不受到MYC状态的影响[4]。Cytarabine（100、500nM）处理敲低了FHL1表达的Kasumi-3和U937细胞72h，具有显著的细胞杀伤作用[5]。
在体内，Cytarabine（200mg/kg）通过腹腔注射治疗急性髓系白血病（AML）模型小鼠，显著提高了小鼠的存活率，从20%提高至59.3%，治疗后残留的白血病细胞表现出了化学抗性[6]。Cytarabine（10mg/kg）通过静脉注射治疗AML模型小鼠，显著提高了小鼠的存活率，与地西他滨联合使用可以增强疗效[7]。
| Cas No. | 147-94-4 | SDF | |
| 别名 | 阿糖胞苷; Cytosine β-D-arabinofuranoside; Cytosine Arabinoside; Ara-C | ||
| 化学名 | 4-amino-1-[(2R,3S,4S,5R)-3,4-dihydroxy-5-(hydroxymethyl)oxolan-2-yl]pyrimidin-2-one | ||
| Canonical SMILES | C1=CN(C(=O)N=C1N)C2C(C(C(O2)CO)O)O | ||
| 分子式 | C9H13N3O5 | 分子量 | 243.2 |
| 溶解度 | Water : 48 mg/mL (197.35 mM) ;DMSO : 17.3 mg/mL (71.13 mM) | 储存条件 | Store at 2-8°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 4.1118 mL | 20.5592 mL | 41.1184 mL |
| 5 mM | 0.8224 mL | 4.1118 mL | 8.2237 mL |
| 10 mM | 0.4112 mL | 2.0559 mL | 4.1118 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
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| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
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2.
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